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WorksheetsCeutics - Exam 1 - Preformulation 1 - Yang
Total questions: 75
Worksheet time: 46mins
Preformulation is the investigation of physicochemical properties of drugs and excipients ______ formulation
before
after
during
Preformulation is a case of
learning before doing
learning as you're doing
learning after doing
Why is preformulation important
foundation of developing robust formulations
foundation of creating already made formulations
What are the goals of preformulation
to establish physical characteristics
to establish the necessary physicochemical parameters of new drug substances
to establish compatibility with common excipients
to determine stability profile
to establish the necessary physicochemical parameters of existing drug substances
A drug is synthesized and tested or screened for pharmacological action. From here, when will the initial preformulation work begin
once there is a sufficient quantity of a compound that has been synthesized to perform initial toxicity studies and analytical work
once there is a minute quantity of a compound that has been synthesized to perform initial toxicity studies and analytical work
What are components of the preliminary evaluation of the preformulation process
compound identity
formula and molecular weight
chemical structure
physical description
toxicity levels
What colors can a preformulation drug have
off-white
cream-yellow
shiny
clear
What types of odors can a preformulation compound have
pungent
sulfurous
fruity
aromatic
rotten
What primary tastes can a preformulation compound have
acidic/sour
bitter
sweet
salty
fruity
Which flavor do chemical structures with H+ have
acidic/sour
bitter
sweet
salty
Which flavor do chemical structures with anions & cations have
acidic/sour
bitter
sweet
salty
Which flavor do chemical structures with high molecular weight salts have
acidic/sour
bitter
sweet
salty
Which flavor do chemical structures with polyhydroxyl compounds, polyhalogenated compounds, and alpha amino acids have
acidic/sour
bitter
sweet
salty
Which equation is this
Stokes-Einstein Equation
Bragg's Law
Index of Refraction (R.I. or n)
Drug Solubility in Ideal Solution
Solubility Prediction
What is the r in this equation
Solvated Radius of Diffusing Solute
Stoke's Radius
Solvent Viscosity
Diffusion Coefficient
Gas Constant
The bigger the Stoke's radius
the smaller the diffusion coefficient; inverse relationship
the larger the diffusion coefficient; complementary relationship
the smaller the diffusion coefficient; complementary relationship
the larger the diffusion coefficient; inverse relationship
What is the D in this equation
Solvated Radius of Diffusing Solute
Stoke's Radius
Solvent Viscosity
Diffusion Coefficient
Gas Constant
What is the R in this equation
Solvated Radius of Diffusing Solute
Stoke's Radius
Solvent Viscosity
Diffusion Coefficient
Gas Constant
What is the n in this equation
Solvated Radius of Diffusing Solute
Stoke's Radius
Solvent Viscosity
Diffusion Coefficient
Gas Constant
Diffusion
is the net movement of molecules/atoms from high concentration to low concentration
is the net movement of molecules/atoms from low concentration to high concentration
results in mixing/mass transport without requiring bulk motion
results in mixing/mass transport with bulk motion
Which drug has the higher molecular weight
Caffeine (194.2 g/mol)
Insulin (41,000 g/mol)
What is the units for diffusion coefficient
cm²/s
K
g/mol
J/mol*K
erg/mol*K
Thermal analysis is a branch of _____ where the properties of materials are studied as they change with temperature
materials science
physical science
thermal science
What is the principle of thermal analysis: change in (1) as a function of (2)
1 - thermal energy; 2 - temperature
1 - temperature; 2 - thermal energy
1 - degrees; 2 - temperature
1 - temperature; 2 - degrees
Thermal analysis utilizes
Differential Scanning Calorimetry (DSC)
Thermogravimetric Analysis (TGA)
Thermomechanical Analysis (TMA)
Melting Point Depression
Polymorphism
What are components of Differential Scanning Calorimetry (DSC)
a thermoanalytical technique
measures the difference in the amount of heat required to increase the temperature of a sample and reference is measured as a function of temperature
measures the difference in the amount of heat required to decrease the temperature of a sample and reference is measured as a function of temperature
a thermogravimetric analysis
What are the types of DSC
Power compensated
Heat flux
Melting point depression
Crystallization
What type of compound can be used during differential scanning calorimetry
compounds that can form crystals
any compound
compounds that are unable to freeze
compounds that are unstable
What represents heat flow during differential scanning calorimetry
dQ/dt
dt/dQ
Tg
Delta H
Crystallization is
exothermic
endothermic
does not use heat
During differential scanning calorimetry, the process of melting a crystal is a(n)
exothermic process
endothermic process
does not use heat
Tg takes place
in the middle of the transition phase
at the beginning of the transition phase
at the end of the transition phase
during Tcrystallization
Thermogravimetric analysis (TGA) is commonly used to determine selected characteristics of materials that exhibit
either mass loss or gain due to decomposition
oxidation
loss of volatiles (such as moisture)
temperature crystals liquify at
What second-order phase transitions can Thermogravimetric Analysis can provide
vaporization
sublimination
aborption
adsorption
desorption
Thermomechanical analysis (TMA) is a measurement of a change of a (1) or a (2) property of the sample against temperature
1 - dimension; 2 - mechanical
1 - mechanical; 2 - dimension
1 - temperature; 2 - physical
1 - phase; 2 - physical
Thermodilatrometry is the measurement of a change of a dimension of the sample with a ____ acting on the sample while it is subjected to a temperature regime
negligible force
strong force
weak force
outside variable
What is the equation for the linear expansion coefficient used in thermomechanical analysis
elongation % / degrees C
degrees C / elongation %
(2 * elongation %) / degrees C
degrees C / (2 * elongation %)
On a thermomechanical analysis graph, where is the Tg point
intersection point of the tangential lines
the first point in the graph
the last point in the graph
the point exactly halfway up the graph
Melting point is affected by and used to determine
the purity of the compound
the strength of the compound
the potency of the compound
The purer the compound, the _____ the melting point range
narrower
higher
shorter
wider
The purer the compound, the _____ the melting point
narrower
higher
shorter
wider
What happens during melting point depression when impurities are present
takes less energy to disrupt the crystal lattice
melting point will be lower
melting point range will be broader
melting point will be higher
melting point range will be narrower
When determining a compound's identity using melting point depression, the unknown is mixed with a little bit of known product. What are correct statements concerning the results
If MP is the same, the compound is pure and the unknown is the known compound
If MP is lower and broader, the compound is either mixed or different
If MP is the same, the compound is impure and the unknown is the known compound
If MP is lower and broader, the compound is pure or mixed
What is a eutectic mixture
one mixture of two compounds has a lower melting point than any other ratio of mixture
one mixture of two compounds has a higher melting point than any other ratio of mixture
one mixture of two compounds has the same melting point as other ratios of mixture
The melting point of a eutectic mixture is
the melting point
the eutectic point
solid A + melting point
solid B + melting point
Polymorphism in materials science is the ability of
a solid material to exist in more than one form or crystal structure
a solid material to exist in one form or crystal structure
a liquid material to exist in more than one form or crystal structure
a liquid material to exist in one form or crystal structure
Differences (1) in the (2) or (3) state
1 - disappear; 2 - liquid; 3 - gas
1 - appear; 2 - liquid; 3 - gas
1 - disappear; 2 - liquid; 3 - solid
1 - appear; 2 - liquid; 3 - solid
Some polymorphs are
metastable and convert to a more stable form
stable and convert to a more metastable form
unstable and unable to maintain a form
Polymorphism is relatively common in
63% barbiturates
67% steroids
40% sulfonamides
50% antihypertensive
Who is the "father of polymorphism"
Walter C. McCrone
Edgar J. Hoover
J. Haleblian
Abbott Park
What are some formulation problems that can occur
polymorphs with certain crystal habits may be difficult to inject in suspension form or to formulate as tablets
transformation between polymorphic forms during storage changes the crystal size in suspensions
crystal growth in creams as a result of phase transformation can cause the cream to become gritty
changes in polymorphic forms of vehicles such as theobroma oil (used for suppositories) could cause products with different and unacceptable melting characteristics
What are characteristics of crystalline solids
have fixed internal structure
have less solubility
less tendency to change its form
tend to revert to more stable form during storage
have greater solubility
What are characteristics of amorphous solids
do not have any fixed internal structure
have less solubility
less tendency to change its form
tend to revert to more stable form during storage
have greater solubility
Which type of drug is more preferred
crystalline solid
amorphous solid
What is an enantiotroph and what is an example of it
when one form is stable over certain pressure and temp range while other polymorph is stable over different pressure and temp range
sulfur
only one polymorph is stable at all temp below the melting pt with all other polymorph being unstable
glyceryl stearate
chloramphenicol palmitate
What is a monotroph and what is an example of it
when one form is stable over certain pressure and temp range while other polymorph is stable over different pressure and temp range
sulfur
only one polymorph is stable at all temp below the melting pt with all other polymorph being unstable
glyceryl stearate
chloramphenicol palmitate
What are some characteristics of an enantiotropic pair
reversible phase transition, endothermic process
lower melting form is thermodynamically stable below the transition temp and higher melting form is stable above the transition temp
higher melting pt has lower heat of fusion
irreversible phase transition, exothermic process
higher melting form is always thermodynamically stable
What are some characteristics of a monotropic pair
reversible phase transition, endothermic process
lower melting form is thermodynamically stable below the transition temp and higher melting form is stable above the transition temp
higher melting pt has higher heat of fusion
irreversible phase transition, exothermic process
higher melting form is always thermodynamically stable
What factors affect polymorphism
temp and humidity
photostability
effect of solvent
effect of grinding
effect of tablet compression
What parameters must be checked by a preformulator when doing a polymorphism study
# of polymorphs, presence of glassy state
stabilization of metastable form, temp of stability range
solubility of polymorph, method of prep
effects of microization, excipients incompatibility
ability to become gritty if needed
What are some technology in polymorphism
optical crystallography, dilatrometry
hot stage microscopy, thermal methods
x-ray diffraction, FTIR technique
dilatometry, microcalorimetry
What is the best way to study polymorphism
optical crystallography
hot stage microscopy, thermal methods
x-ray diffraction
dilatrometry
FTIR technique
What does optical crystallography study
the degree of stability of metastable form
transition temp, melting point
rate of transition under various thermal and physical conditions
whether to pursue polymorphism as a route to an improved dosage form
The index of refraction is a _____ # that describes how light propagates through that material
dimensionless
large
small
nonexistent
What equation is this
Stoke-Einstein Equation
Bragg's Equation
Index of Refraction
Snell's Law of Refraction
What equation is this
Stoke-Einstein Equation
Bragg's Equation
Index of Refraction
Snell's Law of Refraction
For the index in the equation, what is the value of air
n = 1
n > 1
n < 1
n = 0
For the index in the equation, what is the value if it is not air being measured
n = 1
n > 1
n < 1
n = 0
What is this equation and what does it measure
Bragg's Law
Index of Refraction
refractive index
x-ray diffraction
What is FTIR
Fourier Transform Infrared Spectroscopy
Fourier Transform Inverted Spectroscopy
a technique which is used to obtain an infrared spectrum of absorption, emission, photoconductivity or Raman scattering of a solid, liquid, or gas
a technique which is used to obtain an inverted spectrum of absorption, emission, photoconductivity or Raman scattering of a solid, liquid, or gas
In FTIR, what is the only type of sample that can be used in the purpose of polymorph identification
solid
liquid
gas
What are the advantages of using FTIR in polymorph identification
rapid
qualitative
quantitative
accurate
cheap
What are the advantages of using thermal methods in polymorph identification
thermodynamic parameter can be evaluated
heat of transition from one polymorph to the other can be measured
melting point can be determined
heat of fusion from one polymorph to the other can be measured
costs are lowered by not using highly expensive equipment
What is a disadvantage of using DSC and MP determination for polymorph identification
substances undergoing investigation heated through phase transition can decompose
substances undergoing investigation heated through phase transition will not decompose
What is pseudopolymorphism and how do you test for it
solvent molecules get incorporated into the crystal lattice of solids solvates which exist in a different crystal form called pseudopolymorphs
solute molecules get incorporated into the crystal lattice of solids solutes which exist in a different crystal form called pseudopolymorphs
pseudopolymophs bubble when added to solution
pseudopolymophs do not bubble when added to solution
